DH97 is a potent and selective antagonist ofMT₂melatonin receptor, with apK_iof 8.03 for human MT₂. DH97 shows 89- and 229-fold selectivity for human MT₂over human mt₁andXenopusmel_1creceptor subtypes. DH97 can inhibit melatonin-induced enhancement of electrically-evoked responses^[1][2].

DH97 (compound 9) (0.1-100 μM; 2 h) antagonizes pigment aggregation induced by melatonin (10 nM) inXenopus laevismelanophores^[1].
DH97 has no agonist activity at concentrations up to 100 μM^[1].
DH97 (60 nM) significantly alteres the potency of melatonin in the rat tail artery at low concentrations of the MT2 selective ligands, with a pEC₅₀of 8.83^[2].
DH97 (5 μM) causes a significant rightward displacement of the vasoconstrictor effect of melatonin at concentrations non-selective for mt1 and MT₂receptors^[2].

334.45

C₂₂H₂₆N₂O

220339-00-4

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